We screened 95 kinase inhibitors whether they affect cAMP-dependent proteolysis of GATA-6 or not. Among them 7 inhibitors inhibited the proteolysis at the concentration range of μM around their IC50. They are inhibitors for protein kinase A (H-89 and 4cyano-3-methylisoquinoline), c-Jun N-terminal kinase (SP600125), phosphatidylinositol 3-kinase (Wortmannin and LY-294002), casein kinase II (TBB)...

Epidermal growth factor receptor (EGFR) -tyrosine kinase inhibitors (TKI) have transformed traditional cancer treatment and brought good news to patients with non-small cell lung cancer. However, drug resistance problems arise one after another. Based on further exploration of the mechanism EGFR corresponding therapeutic strategies, author reviewed relevant literature, classified summarized it,...

Abstract A reproducible and scalable method has been developed for the synthesis of a series 3,6-substituted pyrazolo[1,5- ]pyrimidines, which are basis rational design selective inhibitors AMP-activated protein kinase. Regarding formation new types carbon skeleton, applicability Suzuki–Miyaura cross-coupling using Buchwald ligands to form C–C bond in sterically hindered position 6 5,7-dimethyl...